106852-87-3

Upstream product

• 110-87-2 3,4-dihydro-2H-pyran 
• 621-59-0 isovanillin 

Downstream Products

• 1215359-56-0 2-[4-(3,4,5-trimethoxystyryl)-2-methoxyphenoxy]tetrahydro-2H-pyran 
• 1215359-55-9 2-[4-(3,4,5-trimethoxystyryl)-2-methoxyphenoxy]tetrahydro-2H-pyran 
• 173534-21-9 1,5-bis(3-hydroxy-4-methoxyphenyl)penta-1,4-dien-3-one 
• 1644568-87-5 C₂₅H₂₈O₆S 
• 2567-65-9 3,2′-dihydroxy-4,4′-dimethoxychalcone 
• 621-59-0 isovanillin 
• 1262430-70-5 (E)-3-(4-methoxy-3-(tetrahydro-2H-pyran-2-yloxy)phenyl)-1-(6-propoxybenzo[d][1,3]oxathiol-5-yl)prop-2-en-1-one 
• 1262429-92-4 (E)-3-(3-hydroxy-4-methoxyphenyl)-1-(6-propoxybenzo[d][1,3]oxathiol-5-yl)prop-2-en-1-one 
• 130600-82-7 1-[2-hydroxy-4-(tetrahydro-pyran-2-yloxy)-phenyl]-3-[4-methoxy-3-(tetrahydro-pyran-2-yloxy)-phenyl]-propenone 
• 1257227-19-2 4-(3'-chloro-4',5'-dimethoxyphenyl)-5-(4''-methoxy-3''-tetrahydropyranyloxyphenyl)-oxazole 
• 1257227-18-1 4-(3'-bromo-4',5'-dimethoxyphenyl)-5-(4''-methoxy-3''-tetrahydropyranyloxyphenyl)-oxazole 

Relevant academic research and scientific papers

NOTCH INHIBITORS FOR USE IN THE TREATMENT OF T-CELL ACUTE LYMPHOBLASTIC LEUKEMIA

Compounds of formula (I) in the capacity of compounds with anti-tumor activity for the treatment of T-cell acute lymphoblastic leukemia (T-ALL).

Functionalized curcumin analogs as potent modulators of the Wnt/β-catenin signaling pathway

Osteosarcoma is a primary bone malignancy with aggressive metastatic potential and poor prognosis rates. In our earlier work we have investigated the therapeutic potential of curcumin as an anti-invasive agent in osteosarcoma by its ability to regulate the Wnt/β-catenin signaling pathway. However, the clinical use of curcumin is limited owing to its low potency and poor pharmacokinetic profile. In this study, an attempt was made to achieve more potent Wnt inhibitory activity in osteosarcoma cells by carrying out synthetic chemical modifications of curcumin. We synthesized a total of five series consisting of 43 curcumin analogs and screened in HEK293T cells for inhibition of β-catenin transcriptional activity. Six promising analogs, which were 6.5- to 60-fold more potent than curcumin in inhibiting Wnt activity, were further assessed for their anti-invasive activity and Wnt inhibitory mechanisms. Western blot analysis showed disruption of β-catenin protein nuclear translocation following treatment with analogs 2f, 3c and 4f. Using transwell assays, we also found that these compounds were more potent than 1a (curcumin) in impeding the invasion of osteosarcoma cells, possibly through suppressing MMP-9 activity. Structure-activity-relationship studies revealed that Wnt inhibitory effects could be enhanced by shortening and restraining the flexibility of the 7-carbon linker moiety connecting the terminal aromatic rings of curcumin and substituting both rings with appropriate substituents. Our results demonstrate that the synthesized curcumin analogs are more potent Wnt inhibitors in osteosarcoma cell lines as compared to parental curcumin and are good lead compounds for further development. Future in vivo tests with these compounds will define their therapeutic potentials as promising drug candidates for clinical treatment of osteosarcoma.

Multitarget-directed benzylideneindanone derivatives: Anti-β-amyloid (Aβ) aggregation, antioxidant, metal chelation, and monoamine oxidase B (MAO-B) inhibition properties against Alzheimer's disease

A novel series of benzylideneindanone derivatives were designed, synthesized, and evaluated as multitarget-directed ligands against Alzheimer's disease. The in vitro studies showed that most of the molecules exhibited a significant ability to inhibit self-induced β-amyloid (Aβ 1-42) aggregation (10.5-80.1%, 20 μM) and MAO-B activity (IC 50 of 7.5-40.5 μM), to act as potential antioxidants (ORAC-FL value of 2.75-9.37), and to function as metal chelators. In particular, compound 41 had the greatest ability to inhibit Aβ1-42 aggregation (80.1%), and MAO-B (IC50 = 7.5 μM) was also an excellent antioxidant and metal chelator. Moreover, it is capable of inhibiting Cu(II)-induced Aβ1-42 aggregation and disassembling the well-structured Aβ fibrils. These results indicated that compound 41 is an excellent multifunctional agent for the treatment of AD.

Solid-Phase Reactive Chromatography (SPRC): A new methodology for wittig and horner-emmons reactions on a column under microwave irradiation

A new methodology named solid-phase reactive chromatography (SPRC), which combines reaction, separation, and purification into a single unit for the preparation of small samples, is described. This method was illustrated in the synthesis of some natural bioactive compounds, namely, methoxylated analogues of resveratrol, alkylresorcinols, and 5-aryl-2,4-pentadienoates, over a column of alumina-KF under microwave irradiation by using the Wittig and HornerEmmons reactions. This approach permitted the preparation of the target olefins with high purity and good to excellent yields in short reaction times.